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Cited by 303Drug Solubulity and Delivery SystemsDrug Transport and Resistance MechanismsCrystallization and Solubility Studies

The DOI matches its Crossref record; 30 of the 32 references it cites were found in a registry or an index.

Estimation of the Increase in Solubility of Drugs as a Function of Bile Salt Concentration

Mithani, Sabena D., Bakatselou, Vassiliki, TenHoor, Christopher N., Dressman, Jennifer B.·1996·Pharmaceutical Research
DOI 10.1023/a:1016062224568
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Abstract

Purpose The objective of this study was to develop a model to predict the extent to which bile salts can enhance the solubility of a drug, based on the physicochemical properties of the compound. The ability to predict bile salt solubilization of poorly soluble drugs would be a key component in determining which drugs will exhibit fed vs. fasted differences in drug absorption.Methods A correlation between the logarithm of the octanol/water partition coefficient [log P] of six steroidal compounds and their solubilities in the presence of various concentrations of sodium taurocholate at 37 degrees C, log [SR] = 2.234 + 0.606 log [P] (r2 = 0.987) where SR is the ratio of the stabilization capacity of the bile salt to the solubilization capacity of water for the drug, was used to predict the solubility of the compounds in presence of sodium taurocholate were then measured.Results The predicted solubilities were within 10% of the experimentally observed solubilities for griseofulvin, cyclosporin A and pentazocine. The model overpredicted the solubility of phenytoin and diazepam in 15 mM sodium taurocholate solution by a factor of 1.33 and 1.62 respectively.Conclusions The expected increase in solubility as a function of bile salt concentration can be estimated on the basis of the partition coefficient and aqueous solubility of the compound.

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Crossref · 10.1023/a:1016062224568

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2 of the 32 references couldn’t be matched to a known paper.

Research works printed but not linked: 1

  1. L. J. M. Naylor. Dissolution mechanisms of poorly soluble compounds in simple and mixed micelle systems. Doctoral Thesis. The University of Michigan. (1993).

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Metadata

Authors
Mithani, S. D., Bakatselou, V., TenHoor, C. N., & Dressman, J. B.
Affiliations
  • University of Michigan (US)
  • Goethe University Frankfurt (DE)
ORCID
Dressman, Jennifer B.
Venue
Pharmaceutical Research
Publisher
Springer Science and Business Media LLC
Published
1996-01
Volume
13
Issue
1
Pages
163-167
ISSN
  • 0724-8741 (ISSN-L)
  • 1573-904X
DOI
10.1023/a:1016062224568
OpenAlex
W1550485225
Cited by
303
References
32
Citations by year
2026: 5 · 2025: 5 · 2024: 8 · 2023: 13 · 2022: 13 · 2021: 11 · 2020: 21 · 2019: 9 · 2018: 14 · 2017: 16 · 2016: 16 · 2015: 12 · 2014: 7 · 2013: 19 · 2012: 11
FWCI
4.95
Type
journal article
Language
en
Open access
closed
Licence
Locations
  • Pharmaceutical Research (publishedVersion)
  • PubMed (publishedVersion)
  • Deep Blue (University of Michigan) (submittedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
  • Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
  • Physical Sciences › Materials Science › Materials Chemistry › Crystallization and Solubility Studies
Keywords
drug solubility enhancement, sodium taurocholate, octanol-water partition coefficient, solubility prediction model, steroids, griseofulvin, cyclosporine, pentazocine, phenytoin, diazepam, poorly water-soluble drugs
MeSH terms
Bile Acids and Salts, Chemistry, Physical, Cholagogues and Choleretics, Diazepam, Fasting, Food, Griseofulvin, Intestinal Absorption, Models, Chemical, Pentazocine, Phenytoin, Solubility, Steroids, Taurocholic Acid, Cyclosporine, Chemical Phenomena

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